Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Hellebore petunidin space isomer compound and preparation and application thereof

A technology of spatial isomers and compounds, which is applied in the field of dienolactone compounds, can solve the problem of few reports of spatial isomers

Inactive Publication Date: 2013-02-27
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] There are more than 250 kinds of such compounds reported so far, but there are very few reports of spatial isomers

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Hellebore petunidin space isomer compound and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1: Preparation of bufadienolactone extract

[0024] Get 5Kg of toad skin and extract 3 times with 95% ethanol, the amount of alcohol used is 10 times, and the extraction time is 120 minutes each time. %-50% ethanol for elution, and then 70%-100% ethanol for elution, collect the latter, recover the solvent under reduced pressure, and dry to obtain 62 g of bufadienolactone extract.

Embodiment 2

[0025] Embodiment 2: Preparation of bufadienolactone fraction

[0026] The bufadienolactone extract obtained in Example 1 was separated by preparative HPLC (XterraC18, A: 0.1% (v / v) formic acid in water; B: 0.1% (v / v) formic acid in acetonitrile, gradient conditions: 5% B to 95% B, 60 min;), during the separation process, an ultraviolet detector is used for detection, and the detection wavelength is 300 nm. Each fraction was collected according to the retention time of different sample peaks during the detection process; a total of 20 fractions (Fraction1-20) were collected.

Embodiment 3

[0027] Embodiment 3: the preparation of compound I

[0028] Fraction 5 reclaims the solvent, separates through HPLC (cyclodextrin chromatographic column, A: n-hexane; B: isopropanol, gradient condition: 5% B ~ 30% B, 55min), collects wherein main chromatographic peak, recovers solvent respectively , determined by NMR experiments, obtained a fraction 3mg containing compound I (peak 3), and the HPLC detection content was 99%, and the rationale was determined. The data are as follows: white powder, HR-MS, [M+H]+(m / z) : 417.2275, UV: 298nm, 1 HNMR (CD 3 OD, 400MHz) δ: 10.12 (1H, s), 8.01 (1H, dd, J=9.6, 1.6), 7.56 (1H, s), 6.43 (1H, d, J=9.6), 3.55 (1H, m) , 2.17(1H, d, J=5.6), 0.78(1H, s), etc.; 13 CNMR (CD 3 OD, 100MHz) δ: 210.2, 167.9, 155.4, 145.1, 133.2, 117.5, 86.2, 70.8, 69.3, 55.7, 51.2, 47.3, 43.2, 42.5, 35.7, 36.8, 31.2, 31.6, 26.3, 25.2, 23.9, 22.4, 19.7.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides a hellebore petunidin space isomer compound and preparation and application thereof. The hellebore petunidin space isomer compound is prepared from the conventional Chinese medicinal toad skin by using macroporous resin and a two-dimensional preparation chromatographic separation technology. The compound is prepared by mainly comprising the following steps of: cutting the toad skin into pieces; extracting with ethanol; separating a total extract by using the macroporous resin to obtain a toad bufadienolides extract; and performing two-dimensional preparation chromatographic separation and purification to obtain the compound. An in-vitro experiment proves that the compound has a good tumor cell suppression effect.

Description

technical field [0001] The present invention relates to diene lactone compounds, specifically a novel compound of helleboregenin space isomers and a preparation method thereof, which is a kind of process developed from traditional Preparation of new compounds isolated from traditional Chinese medicine toad skin. Background technique [0002] Toad is an earlier drug in the clinical application of traditional Chinese medicine, and has a history of clinical application in my country for thousands of years. Its medicinal parts are: skin, toad venom, dry whole. Toad skin has the effect of clearing away heat and detoxifying, diuresis and reducing swelling. It is pungent, cool and slightly poisonous. Acta Pharmaceutica Sinica, 2007, 42(8): 858-861). [0003] Dienolactone compounds are the main active ingredients in toad skin, and modern pharmacological studies have shown that they have cardiotonic, antibacterial, and antitumor effects (Jia Caiyun et al. Chinese Herbal Medicine, ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07J19/00A61K31/585A61P35/00
Inventor 梁鑫淼刘艳芳张秀莉丰加涛肖远胜薛兴亚
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com